CN1170414A - 人中性粒细胞弹性蛋白酶抑制剂 - Google Patents

人中性粒细胞弹性蛋白酶抑制剂 Download PDF

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Publication number
CN1170414A
CN1170414A CN95196952A CN95196952A CN1170414A CN 1170414 A CN1170414 A CN 1170414A CN 95196952 A CN95196952 A CN 95196952A CN 95196952 A CN95196952 A CN 95196952A CN 1170414 A CN1170414 A CN 1170414A
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alkyl
group
methyl
compound
amino
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CN95196952A
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Chinese (zh)
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A·吉尔克斯
L·W·斯普鲁斯
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Cortech Inc
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Cortech Inc
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D271/00—Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms
    • C07D271/02—Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms not condensed with other rings
    • C07D271/10—1,3,4-Oxadiazoles; Hydrogenated 1,3,4-oxadiazoles
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/02—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
    • C07K5/0202—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link containing the structure -NH-X-X-C(=0)-, X being an optionally substituted carbon atom or a heteroatom, e.g. beta-amino acids
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06008—Dipeptides with the first amino acid being neutral
    • C07K5/06017—Dipeptides with the first amino acid being neutral and aliphatic
    • C07K5/06026—Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 0 or 1 carbon atom, i.e. Gly or Ala
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06008—Dipeptides with the first amino acid being neutral
    • C07K5/06017—Dipeptides with the first amino acid being neutral and aliphatic
    • C07K5/06034—Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 2 to 4 carbon atoms
    • C07K5/06043—Leu-amino acid
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06008—Dipeptides with the first amino acid being neutral
    • C07K5/06017—Dipeptides with the first amino acid being neutral and aliphatic
    • C07K5/06034—Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 2 to 4 carbon atoms
    • C07K5/06052—Val-amino acid
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06008—Dipeptides with the first amino acid being neutral
    • C07K5/06078—Dipeptides with the first amino acid being neutral and aromatic or cycloaliphatic
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06086—Dipeptides with the first amino acid being basic
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06104—Dipeptides with the first amino acid being acidic
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06139—Dipeptides with the first amino acid being heterocyclic
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06139—Dipeptides with the first amino acid being heterocyclic
    • C07K5/06156—Dipeptides with the first amino acid being heterocyclic and Trp-amino acid; Derivatives thereof
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06191—Dipeptides containing heteroatoms different from O, S, or N
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08—Tripeptides
    • C07K5/0802—Tripeptides with the first amino acid being neutral
    • C07K5/0804—Tripeptides with the first amino acid being neutral and aliphatic
    • C07K5/0806—Tripeptides with the first amino acid being neutral and aliphatic the side chain containing 0 or 1 carbon atoms, i.e. Gly, Ala
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/12—Cyclic peptides with only normal peptide bonds in the ring
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Molecular Biology (AREA)
  • Genetics & Genomics (AREA)
  • Biophysics (AREA)
  • Biochemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pulmonology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
CN95196952A 1994-11-21 1995-11-17 人中性粒细胞弹性蛋白酶抑制剂 Pending CN1170414A (zh)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US08/345,820 US5618792A (en) 1994-11-21 1994-11-21 Substituted heterocyclic compounds useful as inhibitors of (serine proteases) human neutrophil elastase
US08/345,820 1994-11-21

Publications (1)

Publication Number Publication Date
CN1170414A true CN1170414A (zh) 1998-01-14

Family

ID=23356635

Family Applications (1)

Application Number Title Priority Date Filing Date
CN95196952A Pending CN1170414A (zh) 1994-11-21 1995-11-17 人中性粒细胞弹性蛋白酶抑制剂

Country Status (17)

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US (8) US5618792A (da)
EP (1) EP0793674B1 (da)
JP (1) JPH10511933A (da)
KR (1) KR100369665B1 (da)
CN (1) CN1170414A (da)
AT (1) ATE193304T1 (da)
AU (1) AU687285B2 (da)
CA (1) CA2205198C (da)
DE (1) DE69517196T2 (da)
DK (1) DK0793674T3 (da)
ES (1) ES2145936T3 (da)
GR (1) GR3034208T3 (da)
IL (1) IL116078A (da)
PT (1) PT793674E (da)
TW (1) TW474924B (da)
WO (1) WO1996016080A1 (da)
ZA (1) ZA959819B (da)

Families Citing this family (124)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5618792A (en) * 1994-11-21 1997-04-08 Cortech, Inc. Substituted heterocyclic compounds useful as inhibitors of (serine proteases) human neutrophil elastase
US6001813A (en) * 1994-11-21 1999-12-14 Cortech Inc. Val-pro containing α-keto oxadiazoles as serine protease inhibitors
US6159938A (en) * 1994-11-21 2000-12-12 Cortech, Inc. Serine protease inhibitors comprising α-keto heterocycles
US6100238A (en) * 1994-11-21 2000-08-08 Cortech Inc. Indole and tetrahydroisoquinoline containing Alpha-keto oxadiazoles as serine protease inhibitors
US6001811A (en) * 1994-11-21 1999-12-14 Cortech Inc. Serine protease inhibitors--N-substituted derivatives
US20020119985A1 (en) 1994-11-21 2002-08-29 Albert Gyorkos Serine protease inhibitors
US6015791A (en) * 1994-11-21 2000-01-18 Cortech Inc. Serine protease inhibitors-cycloheptane derivatives
US6001814A (en) * 1994-11-21 1999-12-14 Cortech Inc. Serine protease inhibitors
US6150334A (en) * 1994-11-21 2000-11-21 Cortech, Inc. Serine protease inhibitors-tripeptoid analogs
US5998379A (en) * 1994-11-21 1999-12-07 Cortech Inc. Serine protease inhibitors-proline analogs
DE69633003T2 (de) * 1995-01-27 2005-08-18 Novo Nordisk A/S Verbindungen mit wachstumshormon-freisetzenden eigenschaften
AU2959397A (en) * 1996-05-31 1998-01-05 Novartis Ag Process for the preparation of hydrazine derivatives useful as intermediates for the preparation of peptide analogues
HUP0100669A3 (en) * 1996-12-06 2001-12-28 Cortech Inc Denver Peptide derivatives as serine protease inhibitors, their use and pharmaceutical compositions comprising thereof
US6635632B1 (en) * 1996-12-23 2003-10-21 Athena Neurosciences, Inc. Cycloalkyl, lactam, lactone and related compounds, pharmaceutical compositions comprising same, and methods for inhibiting β-amyloid peptide release and/or its synthesis by use of such compounds
US5773430A (en) * 1997-03-13 1998-06-30 Research Foundation Of State University Of New York Serine proteinase inhibitory activity by hydrophobic tetracycline
AR012374A1 (es) * 1997-04-15 2000-10-18 Smithkline Beecham Corp Inhibidores de proteasas, composiones farmaceuticas y usos para la preparacion de medicamentos.
US6004933A (en) * 1997-04-25 1999-12-21 Cortech Inc. Cysteine protease inhibitors
WO1999016453A1 (en) * 1997-09-26 1999-04-08 Eli Lilly And Company Method for the treatment of cystic fibrosis
US6251930B1 (en) 1997-10-23 2001-06-26 Southern Research Institute Activating C1- secretion
US6656910B2 (en) 1997-12-04 2003-12-02 Cortech, Inc. Serine protease inhibitors
EP1057491B1 (en) * 1998-02-24 2013-06-19 Astellas Pharma Inc. Preventives/remedies for skin aging
US6162791A (en) * 1998-03-02 2000-12-19 Apotex Inc. Thiadiazole compounds useful as inhibitors of cysteine activity dependent enzymes
IL139187A0 (en) * 1998-04-23 2001-11-25 Cortech Inc Cysteine protease inhibitors
EP1093368A4 (en) * 1998-06-03 2002-11-13 Cortech Inc ALPHA KETOOXADIAZOLES CONTAINING INDOL AND TETRAHYDROISOQUINOLINE AS SERINE PROTEASE INHIBITORS
EP1114822A3 (en) * 1998-06-03 2002-11-13 Cortech Inc. Indoles and tetrahydroisoquinolines containing alpha-keto oxadiazoles as serine protease inhibitors
JP2003520185A (ja) * 1998-06-03 2003-07-02 コーテック インコーポレーテッド セリンプロテアーゼ阻害剤としてのα−ケトオキサジアゾール類
DZ2815A1 (fr) * 1998-06-12 2003-12-01 Smithkline Beecham Corp Inhibiteurs de protéase.
US6958330B1 (en) * 1998-06-22 2005-10-25 Elan Pharmaceuticals, Inc. Polycyclic α-amino-ε-caprolactams and related compounds
AUPP508798A0 (en) * 1998-08-05 1998-08-27 Biotech Australia Pty Limited Method of treating psoriasis
AU9031598A (en) * 1998-08-17 2000-03-06 Cortech, Inc. Serine protease inhibitors comprising alpha-keto heterocycles
US6576654B1 (en) 1998-09-23 2003-06-10 Eli Lilly And Company Method for the treatment of cystic fibrosis
WO2000032620A1 (en) 1998-12-02 2000-06-08 Merck Frosst Canada & Co. Gamma-ketoacid tetrapeptides as inhibitors of caspase-3
WO2000051625A1 (en) * 1999-03-05 2000-09-08 The Trustees Of University Technology Corporation Inhibitors of serine protease activity, methods and compositions for treatment of herpes viruses
WO2000051624A2 (en) * 1999-03-05 2000-09-08 The Trustees Of University Technology Corporation Methods and compositions useful in inhibiting apoptosis
US6849605B1 (en) * 1999-03-05 2005-02-01 The Trustees Of University Technology Corporation Inhibitors of serine protease activity, methods and compositions for treatment of viral infections
AU3511500A (en) 1999-03-05 2000-09-21 Trustees Of University Technology Corporation, The Inhibitors of serine protease activity, methods and compositions for treatment of nitric oxide-induced clinical conditions
NZ513921A (en) * 1999-03-12 2001-09-28 Ono Pharmaceutical Co 1,3,4-oxadiazole derivatives and process for producing the same
US7276348B2 (en) * 1999-04-30 2007-10-02 Regents Of The University Of Michigan Compositions and methods relating to F1F0-ATPase inhibitors and targets thereof
US20040176358A1 (en) * 1999-04-30 2004-09-09 The Regents Of The University Of Michigan Compositions and methods relating to novel compounds and targets thereof
US20060025388A1 (en) 1999-04-30 2006-02-02 Glick Gary D Compositions and methods relating to novel compounds and targets thereof
US20050113460A1 (en) * 1999-04-30 2005-05-26 The Regents Of The University Of Michigan Compositions and methods relating to novel compounds and targets thereof
US20030119029A1 (en) * 1999-04-30 2003-06-26 Regents Of The University Of Michigan Compositions and methods relating to novel benzodiazepine compounds and targets thereof
EP1143946B1 (en) 1999-04-30 2004-01-28 The Regents Of The University Of Michigan Use of benzodiazepines for treating autoimmune diseases induced by apoptosis
US7144880B2 (en) 1999-04-30 2006-12-05 Regents Of The University Of Michigan Compositions relating to novel compounds and targets thereof
US6908919B2 (en) * 1999-05-19 2005-06-21 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl pyrazinones useful for selective inhibition of the coagulation cascade
US6664255B1 (en) * 1999-05-19 2003-12-16 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl pyrazinones useful for selective inhibition of the coagulation cascade
US6867217B1 (en) 1999-05-19 2005-03-15 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl pyridones useful for selective inhibition of the coagulation cascade
US7015230B1 (en) 1999-05-19 2006-03-21 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl uracils useful for selective inhibition of the coagulation cascade
US6750342B1 (en) * 1999-05-19 2004-06-15 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl pyrimidinones useful for selective inhibition of the coagulation cascade
US6716838B1 (en) 1999-05-19 2004-04-06 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl uracils as anticoagulative agents
US6653316B1 (en) 1999-05-19 2003-11-25 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl pyrimidinones useful for selective inhibition of the coagulation cascade
US6906068B1 (en) 1999-05-19 2005-06-14 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl 1,2,4 - triazinones useful as anticoagulants
US6458952B1 (en) 1999-05-19 2002-10-01 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl uracils useful for selective inhibition of the coagulation cascade
AU5625900A (en) * 1999-06-17 2001-01-09 Cortech, Inc. Method and compounds for inhibiting activity of serine elastases
US7122627B2 (en) * 1999-07-26 2006-10-17 Bristol-Myers Squibb Company Lactam inhibitors of Hepatitis C virus NS3 protease
EP1206449A1 (en) * 1999-07-26 2002-05-22 Bristol-Myers Squibb Company Lactam inhibitors of hepatitis c virus ns3 protease
US6358928B1 (en) 1999-11-22 2002-03-19 Enzyme Systems Products Peptidyl sulfonyl imidazolides as selective inhibitors of serine proteases
AR026748A1 (es) * 1999-12-08 2003-02-26 Vertex Pharma Un compuesto inhibidor de caspasas, una composicion farmaceutica que lo comprende, un metodo para la sintesis del mismo y un compuesto intermediario paradicha sintesis
US6448278B2 (en) * 1999-12-23 2002-09-10 Pfizer Inc. Procollagen C-proteinase inhibitors
AU2001243598A1 (en) 2000-03-13 2001-09-24 Pharmacia Corporation Polycyclic aryl and heteroaryl substituted benzenes useful for selective inhibition of the coagulation cascade
US6875791B2 (en) 2000-04-05 2005-04-05 Pharmacia Corporation Polycyclic aryl and heteroaryl substituted 4-pyrones useful for selective inhibition of the coagulation cascade
AU2001251315A1 (en) * 2000-04-05 2001-10-23 Pharmacia Corporation Polycyclic aryl and heteroaryl substituted 4-pyridones useful for selective inhibition of the coagulation cascade
US20040171616A9 (en) 2000-04-17 2004-09-02 South Michael S. Polycyclic aryl and heteroaryl substituted 1,4-quinones useful for selective inhibition of the coagulation cascade
AU2001222501A1 (en) * 2000-05-18 2001-11-26 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl pyrimidinones useful for selective inhibition of the coagulation cascade
CA2416248A1 (en) 2000-07-18 2002-01-24 Neurogen Corporation 5-substituted 2-aryl-4-pyrimidinones
CA2423945A1 (en) * 2000-09-29 2003-03-27 Atsushi Nagai Restrainers of airway mucus secretion
KR20030046469A (ko) * 2000-09-29 2003-06-12 오노 야꾸힝 고교 가부시키가이샤 염증성 장질환 치료제
WO2002042272A2 (en) 2000-11-20 2002-05-30 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl pyridines useful for selective inhibition of the coagulation cascade
US7119094B1 (en) 2000-11-20 2006-10-10 Warner-Lambert Company Substituted polycyclic aryl and heteroarpyl pyrazinones useful for selective inhibition of the coagulation cascade
US7015223B1 (en) 2000-11-20 2006-03-21 Pharmacia Corporation Substituted polycyclic aryl and heteroaryl 1,2,4-triazinones useful for selective inhibition of the coagulation cascade
WO2002062797A2 (en) * 2000-12-29 2002-08-15 Celltech R & D, Inc. Pharmaceutical uses and synthesis of diketopiperazines
US6645993B2 (en) * 2001-03-30 2003-11-11 Warner-Lambert Company 3-heterocyclylpropanohydroxamic acid PCP inhibitors
US20030236257A1 (en) * 2001-04-04 2003-12-25 South Michael S. Polycyclic aryl and heteroaryl substituted 4-pyridones useful for selective inhibition of the cogulation cascade
DE60234028D1 (de) * 2001-05-25 2009-11-26 Bristol Myers Squibb Co Hydantion-derivate als hemmer von matrix-metalloproteinasen
WO2003006014A1 (en) * 2001-07-10 2003-01-23 Ono Pharmaceutical Co., Ltd. Medicine comprising combination of five-membered heterocyclic compound and drug compensating for or enhancing its activity
EP1448534A1 (en) * 2001-10-03 2004-08-25 Pharmacia Corporation 6-membered unsaturated heterocyclic compounds useful for selective inhibition ofthe coagulation cascade
AU2002367752A1 (en) * 2001-10-03 2003-11-17 Pharmacia Corporation Substituted 5-membered polycyclic compounds useful for selective inhibition of the coagulation cascade
WO2003029216A1 (en) * 2001-10-03 2003-04-10 Pharmacia Corporation 6-membered heterocyclic compounds useful for selective inhibition of the coagulation cascade
US20040082585A1 (en) * 2001-10-03 2004-04-29 Pharmacia Corporation Prodrugs of substituted polycyclic compounds useful for selective inhibition of the coagulation cascade
US7884182B2 (en) * 2001-11-14 2011-02-08 Amylin Pharmaceuticals, Inc. Chemical peptide ligation with three or more components
US20040068113A1 (en) * 2001-11-20 2004-04-08 South Michael S. Substituted polycyclic aryl and heteroaryl pyridines useful for selective inhibition of the coagulation cascade
WO2003047740A2 (en) * 2001-12-05 2003-06-12 California Institute Of Technology ENANTIOSELECTIVE TRANSFORMATION OF α,β-UNSATURATED KETONES USING CHIRAL ORGANIC CATALYSTS
US7127063B2 (en) * 2001-12-31 2006-10-24 Certicom Corp. Method and apparatus for computing a shared secret key
US7344700B2 (en) * 2002-02-28 2008-03-18 University Of Tennessee Research Corporation Radiolabeled selective androgen receptor modulators and their use in prostate cancer imaging and therapy
US20040018984A1 (en) * 2002-07-17 2004-01-29 Mizuo Miyazaki Methods for preventing adhesion formation using protease inhibitors
TW200418791A (en) * 2003-01-23 2004-10-01 Bristol Myers Squibb Co Pharmaceutical compositions for inhibiting proteasome
US20040220242A1 (en) * 2003-05-02 2004-11-04 Leland Shapiro Inhibitors of serine protease activity, methods and compositions for treatment of nitric oxide induced clinical conditions
US7405210B2 (en) * 2003-05-21 2008-07-29 Osi Pharmaceuticals, Inc. Pyrrolopyridine-2-carboxylic acid amide inhibitors of glycogen phosphorylase
US7059806B2 (en) * 2003-08-21 2006-06-13 Trangsrud Julian P Hole former for an invert
US7850970B2 (en) * 2003-08-26 2010-12-14 The Regents Of The University Of Colorado Inhibitors of serine protease activity and their use in methods and compositions for treatment of bacterial infections
EP1725555B1 (en) 2004-03-08 2010-10-06 Prosidion Ltd. Pyrrolopyridine-2-carboxylic acid hydrazides as inhibitors of glycogen phosphorylase
US20050272723A1 (en) * 2004-04-27 2005-12-08 The Regents Of The University Of Michigan Methods and compositions for treating diseases and conditions associated with mitochondrial function
US7453002B2 (en) 2004-06-15 2008-11-18 Bristol-Myers Squibb Company Five-membered heterocycles useful as serine protease inhibitors
US20060052369A1 (en) * 2004-09-07 2006-03-09 The Regents Of The University Of Michigan Compositions and methods relating to novel compounds and targets thereof
WO2006059164A2 (en) 2004-12-02 2006-06-08 Prosidion Limited Pyrrolopyridine-2-carboxylic acid amides
AU2006203946B2 (en) * 2005-01-03 2009-07-23 The Regents Of The University Of Michigan Compositions and methods relating to novel compounds and targets thereof
US20070043033A1 (en) * 2005-06-01 2007-02-22 The Regents Of The University Of Michigan Unsolvated benzodiazepine compositions and methods
US20070105844A1 (en) * 2005-10-26 2007-05-10 Regents Of The University Of Michigan Therapeutic compositions and methods
EP2604269B1 (en) 2005-11-01 2014-09-24 The Regents Of The University Of Michigan 1,4-benzodiazepine-2,5-diones with therapeutic properties
US20080124303A1 (en) * 2005-12-12 2008-05-29 Cavit Sciences, Inc Methods and compositions for treatment of viral infections
US7759338B2 (en) * 2006-04-27 2010-07-20 The Regents Of The University Of Michigan Soluble 1,4 benzodiazepine compounds and stable salts thereof
KR101069051B1 (ko) * 2006-05-23 2011-09-29 아이알엠 엘엘씨 채널 활성화 프로테아제 억제제로서의 화합물 및 조성물
AU2007258468B2 (en) 2006-06-09 2011-09-22 The Regents Of The University Of Michigan Compositions and methods relating to novel compounds and targets thereof
BRPI0807483A2 (pt) 2007-02-09 2014-05-13 Irm Llc Compostos e composições como inibidores de protease de ativação de canal
MX2009008493A (es) * 2007-02-09 2009-08-20 Irm Llc Compuestos y composiciones como inhibidores de la proteasa activadora de canal.
KR101131238B1 (ko) 2007-02-09 2012-03-30 아이알엠 엘엘씨 채널 활성화 프로테아제 억제제로서의 화합물 및 조성물
MX2009009645A (es) 2007-03-09 2009-11-19 Univ Michigan Composiciones y metodos relacionados con nuevos compuestos y objetivos de los mismos.
WO2008141081A1 (en) * 2007-05-10 2008-11-20 Amr Technology, Inc. Aryl- and heteroaryl-substituted tetrahydrobenzo-1,4-diazepines and use thereof to block reuptake of norepinephrine, dopamine, and serotonin
WO2009036175A2 (en) 2007-09-14 2009-03-19 The Regents Of The University Of Michigan F1f0-atpase inhibitors and related methods
CN101918375A (zh) 2007-11-06 2010-12-15 密歇根大学董事会 在皮肤病症的治疗中有用的苯并二氮杂*酮化合物
US20090156509A1 (en) * 2007-12-12 2009-06-18 Accuthera, Inc. Tri-peptide Inhibitors of Serine Elastases
JP5567573B2 (ja) 2008-09-11 2014-08-06 ザ リージェンツ オブ ザ ユニバーシティ オブ ミシガン アリールグアニジンｆ１ｆ０−ａｔｐアーゼ阻害剤およびそれと関連する方法
US8604023B2 (en) 2009-04-17 2013-12-10 The Regents Of The University Of Michigan 1,4-benzodiazepinone compounds and their use in treating cancer
JP2013505258A (ja) 2009-09-18 2013-02-14 ザ リージェンツ オブ ザ ユニバーシティ オブ ミシガン ベンゾジアゼピノン化合物およびそれを使用する治療方法
AU2010322286B2 (en) 2009-11-17 2014-06-05 The Regents Of The University Of Michigan 1,4-benzodiazepine-2,5-diones and related compounds with therapeutic properties
WO2011062766A2 (en) 2009-11-17 2011-05-26 The Regents Of The University Of Michigan 1,4-benzodiazepine-2,5-diones and related compounds with therapeutic properties
MX2012006877A (es) * 2009-12-18 2012-08-31 Idenix Pharmaceuticals Inc Inhibidores de virus de hepatitis c de arileno o heteroarileno 5, 5 - fusionado.
EP2723370A4 (en) 2011-06-24 2015-06-03 Univ Colorado Regents COMPOSITIONS, PROCESS AND USE OF ALPHA-1-ANTITRYPHIN FUSION MOLECULES
WO2013026015A1 (en) 2011-08-18 2013-02-21 Dana-Farber Cancer Institute, Inc. Muc1 ligand traps for use in treating cancers
KR20140137347A (ko) 2012-01-10 2014-12-02 더 리젠츠 오브 더 유니버시티 오브 콜로라도, 어 바디 코포레이트 알파-1 안티트립신 융합 분자용 조성물, 방법 및 용도
ES2645847T3 (es) 2013-05-08 2017-12-11 Kissei Pharmaceutical Co., Ltd. Derivado de glicinamida alfa-sustituido
JP2023500182A (ja) 2019-09-17 2023-01-05 メレオ バイオファーマ ４ リミテッド 移植片拒絶反応、閉塞性細気管支炎症候群、及び移植片対宿主病の治療に使用するためのアルベレスタット
EP4106757B1 (en) 2020-04-16 2023-08-23 Mereo Biopharma 4 Limited Methods involving neutrophil elastase inhibitor alvelestat for treating respiratory disease mediated by alpha-1 antitrypsin deficiency
TW202325294A (zh) 2021-10-20 2023-07-01 英商梅瑞奧生物製藥４有限公司 用於治療纖維化之嗜中性球彈性蛋白酶抑制劑

Family Cites Families (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB397073A (en) * 1932-06-09 1933-08-17 Solex Improvements in carburettors for internal combustion engines
GB1397073A (en) * 1971-05-19 1975-06-11 Glaxo Lab Ltd 1,2,4-oxadizoles
US4338453A (en) * 1980-09-17 1982-07-06 The Upjohn Company Aminoalkyl-1,2,4-triazoles
US5055450A (en) * 1985-01-22 1991-10-08 Ici Americas Inc. Peptide derivatives
GB8809316D0 (en) * 1987-05-11 1988-05-25 Ici America Inc Heterocyclic ketones
EP0376012A3 (en) * 1988-12-27 1992-05-06 American Cyanamid Company Renin inhibitors
EP0480044A4 (en) * 1990-03-30 1993-06-09 Japan Tobacco Inc. Novel 4h-3,1-benzoxazin-4-one derivative
GB9216272D0 (en) * 1991-08-15 1992-09-09 Ici Plc Substituted heterocycles
AU655831B2 (en) * 1991-08-22 1995-01-12 Merrell Pharmaceuticals Inc. Novel orally-active elastase inhibitors
GB9307555D0 (en) * 1992-04-16 1993-06-02 Zeneca Ltd Heterocyclic compounds
FR2694295B1 (fr) * 1992-07-28 1994-09-02 Adir Nouveaux peptides dérivés de trifluoromethylcetones, leur procéde de préparation et les compositions pharmaceutiques qui les contiennent.
US5550139A (en) * 1994-01-03 1996-08-27 The Wichita State University Serine protease inhibitors
GB9402680D0 (en) * 1994-02-11 1994-04-06 Zeneca Ltd Pyrrolidine derivatives
US6008196A (en) * 1994-06-02 1999-12-28 Hoechst Marion Roussel, Inc. Perfluoroalkyl ketone inhibitors of elastase and processes for making the same
US5618792A (en) * 1994-11-21 1997-04-08 Cortech, Inc. Substituted heterocyclic compounds useful as inhibitors of (serine proteases) human neutrophil elastase

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